Tetrazole-Based Probes for Integrated Phenotypic Screening, Affinity-Based Proteome Profiling, and Sensitive Detection of a Cancer Biomarker

Title
Tetrazole-Based Probes for Integrated Phenotypic Screening, Affinity-Based Proteome Profiling, and Sensitive Detection of a Cancer Biomarker
Authors
이준석Ke ChengPiliang HaoShao Q. YaoKe DingZhengqiu Li
Keywords
affinity-based probes; cancer biomarkers; target identification
Issue Date
2017-11
Publisher
Angewandte Chemie international edition
Citation
VOL 56, NO 47-15048
Abstract
Target-identification phenotypic screening has been a powerful approach in drug discovery; however, it is hindered by difficulties in identifying the underlying cellular targets. To address this challenge, we have combined phenotypic screening of a fully functionalized small-molecule library with competitive affinity-based proteome profiling to map and functionally characterize the targets of screening hits. Using this approach, we identified ANXA2, PDIA3/4, FLAD1, and NOS2 as primary cellular targets of two bioactive molecules that inhibit cancer cell proliferation. We further demonstrated that a panel of probes can label and/or image annexin A2 (a cancer biomarker) from different cancer cell lines, thus providing opportunities for potential cancer diagnosis and therapy.
URI
http://pubs.kist.re.kr/handle/201004/66605
ISSN
1433-7851
Appears in Collections:
KIST Publication > Article
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